Usherwood P N R, Vais H, Khambay B P S, Davies T G E, Williamson M S
School of Biology, The University of Nottingham, Nottingham, NG7 2RD, UK.
FEBS Lett. 2005 Nov 21;579(28):6317-25. doi: 10.1016/j.febslet.2005.09.096. Epub 2005 Oct 21.
DDT inhibits Na channel inactivation and deactivation, promotes Na channel activation and reduces the resting potential of Xenopus oocytes expressing the Drosophila para Na channel. These changes are only marginally influenced by the single mutation M918T (super-kdr) but are reduced approximately 10-fold by either the single mutation L1014F (kdr) or the double mutation L1014F+M918T, both of which confer resistance to the pyrethroids permethrin and deltamethrin. We conclude that DDT binds either to or in the region of L1014 on IIS6 but only weakly to M918 on the IIS4-S5 linker, which is part of a high-affinity binding site for permethrin and deltamethrin.
滴滴涕抑制蛙卵母细胞中表达果蝇para钠通道的钠通道失活和去激活,促进钠通道激活,并降低其静息电位。这些变化仅受到单一突变M918T(超级抗性家蝇击倒抗性)的轻微影响,但单一突变L1014F(家蝇击倒抗性)或双重突变L1014F+M918T可使其降低约10倍,这两种突变均赋予对拟除虫菊酯氯菊酯和溴氰菊酯的抗性。我们得出结论,滴滴涕要么与位于IIS6上的L1014区域结合,要么与该区域内结合,但仅与IIS4-S5连接体上的M918弱结合,而IIS4-S5连接体是氯菊酯和溴氰菊酯高亲和力结合位点的一部分。